BCTC

产品说明书

Print
Chemical Structure| 393514-24-4 同义名 : -
CAS号 : 393514-24-4
货号 : A224797
分子式 : C20H25ClN4O
纯度 : 99%+
分子量 : 372.89
MDL号 : MFCD08690556
存储条件：

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells. BCTC exerts an anti-proliferative effect on DU145 cells and induces tumor suppression through G0/G1 cell cycle arrest, and inhibition of migration and invasion. BCTC demonstrates excellent anti-tumor activity in PCa DU145 cells, and therefore has the potential to become a targeted therapeutic strategy against PCa[3]. Administration of BCTC (30 mg/kg p.o.) significantly reduced both mechanical and thermal hyperalgesia induced by intraplantar injection of 30 micro g of capsaicin. In rats with Freund's complete adjuvantinduced inflammation, BCTC significantly reduced the accompanying thermal and mechanical hyperalgesia (3 mg/kg and 10 mg/kg p.o., respectively). BCTC also reduced mechanical hyperalgesia and tactile allodynia 2 weeks after partial sciatic nerve injury (10 and 30 mg/kg p.o.)[4]. Moreover, of the TRPV-1 receptor antagonists studied, BCTC (1μM) seems the most reliable in isolated organ experiments. This substance is also effective in the human intestine[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.68mL

0.54mL

0.27mL

13.41mL

2.68mL

1.34mL

26.82mL

5.36mL

2.68mL
参考文献

[1]Liu T, Fang Z, et al. Anti-tumor activity of the TRPM8 inhibitor BCTC in prostate cancer DU145 cells. Oncol Lett. 2016 Jan;11(1):182-188.

[2]Pomonis JD, Harrison JE, et al. N-(4-Tertiarybutylphenyl)-4-(3-cholorphyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: II. in vivo characterization in rat models of inflammatory and neuropathic pain. J Pharmacol Exp Ther. 2003 Jul;306(1):387-93.

[3]Liu T, Fang Z, Wang G, Shi M, Wang X, Jiang K, Yang Z, Cao R, Tao H, Wang X, Zhou J. Anti-tumor activity of the TRPM8 inhibitor BCTC in prostate cancer DU145 cells. Oncol Lett. 2016 Jan;11(1):182-188

[4]Pomonis JD, Harrison JE, Mark L, Bristol DR, Valenzano KJ, Walker K. N-(4-Tertiarybutylphenyl)-4-(3-cholorphyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: II. in vivo characterization in rat models of inflammatory and neuropathic pain. J Pharmacol Exp Ther. 2003 Jul;306(1):387-93

[5]Benko R, Illényi L, Kelemen D, Papp R, Papp A, Bartho L. Use and limitations of three TRPV-1 receptor antagonists on smooth muscles of animals and man: a vote for BCTC. Eur J Pharmacol. 2012 Jan 5;674(1):44-50